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Its activation involves binding of endogenous ligands (such as polyunsaturated fatty acids and prostaglandin derivatives) or synthetic agonists (such as thiazolidinediones) to the receptor, which promotes the formation of a heterodimer with the retinoid X receptor

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ARG BPC-157 to sól argininowa pentadekapeptydu o sekwencji Gly-Glu-Pro-Pro-Pro-Gly-Lys-Pro-Ala-Asp-Asp-Ala-Gly-Leu-Val (zapis jednoliterowy: GEPPPGKPADDAGLV ), wzór sumaryczny rdzenia C₆₂H₉₈N₁₆O₂₂ , masa molowa wolnego peptydu 1419,53 g/mol , numer CAS 137525-51-0